Inhibitors of integrin vla-4
AssigneeMolecular Insight Pharmaceuticals, Inc.
InventorsCraig N. ZIMMERMAN, John W. BABICH
Life of this patent
Estimating the term…
Abstract
A complex, its stereoisomer or pharmaceutically acceptable salt has the formula I, where: wherein: W is a group that is A, B, or C: R1 is hydrogen, alkyl or alkoxy; R2 is a bond, hydrogen or alkyl R3, R4 and R5 are independently hydrogen, iodine, alkyl, alkoxy, hydroxyl, amino, aminoalkyl, dialkylamino, or carboxyl; X is a bond, C═O, O═C—O, or CH2; Y is a bond, CH2, or O; m is an integer ranging from 1 to 6; n is an integer ranging from 0 to 6; Metal represents a metallic moiety comprising a radionuclide; and Chelate represents a chelating moiety that coordinates with said radionuclide to form the complex.
Claims21
A complex of formula I, its stereoisomer or pharmaceutically acceptable salt:
- wherein:
- W is a group that is A, B, or C:
- R1 is hydrogen, alkyl or alkoxy;
- R2 is a bond, hydrogen or alkyl;
- R3, R4 and R5 are independently hydrogen, iodine, alkyl, alkoxy, hydroxyl, amino, aminoalkyl, dialkylamino, or carboxyl;
- X is a bond, C═O, O═C—O, or CH2;
- Y is a bond, CH2, or O;
- m is an integer ranging from 1 to 6;
- n is an integer ranging from 0 to 6;
- Metal represents a metallic moiety comprising a radionuclide;
- and
- Chelate represents a chelating moiety that coordinates with said radionuclide to form the complex.
A method of imaging tissue of a mammal which expresses VLA-4 comprising administering to said mammal an effective amount of a complex of formula I, its stereoisomer or pharmaceutical salt:
- wherein:
- W is a group that is A, B, or C:
- R1 is hydrogen, alkyl or alkoxy;
- R2 is a bond, hydrogen or alkyl;
- R3, R4 and R5 are independently hydrogen, iodine, alkyl, alkoxy, hydroxyl, amino, aminoalkyl, dialkylamino, or carboxyl;
- X is a bond, C═O, O═C—O, or CH2;
- Y is a bond, CH2, or O;
- m is an integer ranging from 1 to 6;
- n is an integer ranging from 0 to 6;
- Metal represents a metallic moiety comprising a radionuclide;
- and
- Chelate represents a chelating moiety that coordinates with said radionuclide to form the complex.
A method of treating a mammal suffering a disease which is characterized by overexpression of VLA-4, the method comprising administering to said mammal a therapeutically effective amount of a complex of formula I, its stereoisomer or pharmaceutical salt:
- wherein:
- W is a group that is A, B, or C:
- R1 is hydrogen, alkyl or alkoxy;
- R2 is a bond, hydrogen or alkyl;
- R3, R4 and R5 are independently hydrogen, iodine, alkyl, alkoxy, hydroxyl, amino, aminoalkyl, dialkylamino, or carboxyl;
- X is a bond, C═O, O═C—O, or CH2;
- Y is a bond, CH2, or O;
- m is an integer ranging from 1 to 6;
- n is an integer ranging from 0 to 6;
- Metal represents a metallic moiety comprising a radionuclide;
- and
- Chelate represents a chelating moiety that coordinates with said radionuclide to form the complex.
A kit comprising a complex of formula I, its stereoisomer or pharmaceutical salt:
- wherein:
- W is a group that is A, B, or C:
- R1 is hydrogen, alkyl or alkoxy;
- R2 is a bond, hydrogen or alkyl;
- R3, R4 and R5 are independently hydrogen, iodine, alkyl, alkoxy, hydroxyl, amino, aminoalkyl, dialkylamino, or carboxyl;
- X is a bond, C═O, O═C—O, or CH2;
- Y is a bond, CH2, or O;
- m is an integer ranging from 1 to 6;
- n is an integer ranging from 0 to 6;
- Metal represents a metallic moiety comprising a radionuclide;
- Chelate represents a chelating moiety that coordinates with said radionuclide to form the complex;
- and
- a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.